Synthesis and preliminary anti-inflammatory and anti-bacterial evaluation of some diflunisal aza-analogs
()
Med. Chem. Commun., 2018, Advance Article
DOI: 10.1039/C8MD00139A, Research Article
Davide Carta, Paola Brun, Matteo Dal Pra, Giulia Bernabe, Ignazio Castagliuolo, Maria Grazia Ferlin
The new diflunisal aza-analogs multi-target approach is remarkable in the treatment of infections induced by multi-drug resistant bacteria. Diflunisal aza-analogs preserved the anti-inflammatory
activity and significantly potentiated the antimicrobial activity of antibiotics.
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Pharmacophore-based tailoring of biphenyl amide derivatives as selective 5-hydroxytryptamine 2B receptor antagonists
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Med. Chem. Commun., 2018, Accepted Manuscript
DOI: 10.1039/C8MD00204E, Research Article
Moustafa Tarek Gabr, Mohammed Abdel-Raziq
We designed and synthesized a new biphenyl amide-tryptamine hybrid molecule 7 utilizing a pharmacophore-based approach as 5-HT2B antagonist. The hybrid compound 7 was evaluted for its affinity to
a panel...
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Assessment of the trifluoromethyl ketone functionality as an alternative zinc-binding group for selective HDAC6 inhibition
()
Med. Chem. Commun., 2018, Advance Article
DOI: 10.1039/C8MD00107C, Research Article
Yves Depetter, Silke Geurs, Flore Vanden Bussche, Rob De Vreese, Jorick Franceus, Tom Desmet, Olivier De Wever, Matthias D'hooghe
The replacement of the hydroxamic acid zinc-binding group in benzohydroxamic acid HDAC6 inhibitors by a trifluoromethyl ketone function leads to severe reduction in enzymatic and cellular
activity.
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Novel 99mTc labelled complexes with 2-nitroimidazole isocyanide: design, synthesis and evaluation as potential tumor hypoxia imaging agents
()
Med. Chem. Commun., 2018, Advance Article
DOI: 10.1039/C8MD00146D, Research Article
Qing Ruan, Xuran Zhang, Xiao Lin, Xiaojiang Duan, Junbo Zhang
99m Tc-2c can be prepared by a direct labelling method without the need for heating and would be a promising probe for hypoxia imaging.
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Design and Synthesis of Novel 1,3,5-Triphenyl Pyrazolines as Potential Anti-Inflammatory Agents Through Allosteric Inhibition of Protein Kinase Czeta (PKC[small zeta])
()
Med. Chem. Commun., 2018, Accepted Manuscript
DOI: 10.1039/C8MD00100F, Research Article
Mohammad Abdel-Halim, Ashraf H. Abadi, Matthias Engel
Much light has been shed on the vital role of Czeta (PKC[small zeta]) in NF-[small kappa]B activation and the potential use of PKC[small zeta] inhibitors as anti-inflammatory agents. We
previously reported the class...
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Isolation, expression and biochemical characterization of recombinant hyoscyamine-6[small beta]-hydroxylase from Brugmansia sanguinea - tuning the scopolamine production
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Med. Chem. Commun., 2018, Advance Article
DOI: 10.1039/C8MD00090E, Research Article
Conrad Fischer, Moonhyuk Kwon, Dae-Kun Ro, Marco J. van Belkum, John C. Vederas
Using a stabilizing small ubiquitin like modifier (SUMO) fusion, a new homologue of hyoscyamine-6[small beta]-hydroxylase from Brugmansia sanguinea (BsH6H) boosts scopolamine
production.
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Elucidation of fluorine's impact on pKa and in vitro Pgp-mediated efflux for a series of PDE9 inhibitors
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Med. Chem. Commun., 2018, Advance Article
DOI: 10.1039/C8MD00114F, Research Article
Kasper Fjelbye, Mauro Marigo, Rasmus P. Clausen, Erling B. Jorgensen, Claus T. Christoffersen, Karsten Juhl
The influence of replacing a hydrogen atom with fluorine on the pKa and Pgp-mediated efflux is elucidated for a series of PDE9 inhibitors.
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Design, synthesis and antimicrobial activity of usnic acid derivatives
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Med. Chem. Commun., 2018, Advance Article
DOI: 10.1039/C8MD00076J, Research Article
Kartsev Victor, Lichitsky Boris, Geronikaki Athina, Petrou Anthi, Smiljkovic Marija, Kostic Marina, Radanovic Oliver, Sokovic Marina
Usnic acid, a dibenzofuran, was originally isolated from lichens producing secondary metabolites, and is well known as an antibiotic, but is also endowed with several other interesting
properties.
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